期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 8, 期 10, 页码 922-934出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802608784911653
关键词
3-quinolinecarbonitrile; kinase; Src; cancer; Abl; CML; SKI-606; bosutinib
In 2000, Wyeth reported that the 3-quinolinecarbonitrile ring system was a template for EGFR inhibitors. It soon became apparent that the group at C-4 of this core was responsible for kinase selectivity. A 4-(2,4-dichloro-5-methoxyanilino) substituent provided potent inhibitors of Src, a non-receptor tyrosine kinase that plays a key role in cell signaling. One compound from this series, SKI-606, bosutinib, is currently in clinical trials for the treatment of cancer.
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